Hydrazine → HCID 66936083, compound

Participants

Reaction Steps

4,6-Dichloro-2-(difluoromethyl)-5-fluoropyrimidine (200 mg, 0.92 mmol) was dissolved in DMSO (5 mL) and stirred at room temperature. N-methylpiperazine (110 μL, 0.96 mmol) was added, followed by DIPEA (500 μL, 2.9 mmol). The resulting mixture was stirred at room temperature for 1 hour, until the N-methylpiperazine displacement of one chlorine was complete as determined by LCMS. Hydrazine (1 mL, 31 mmol) was added and the reaction was stirred overnight at room temperature. The crude reaction mixture was purified by RP-HPLC to provide 2-(difluoromethyl)-5-fluoro-4-hydrazino-6-(4-methyl-1-piperazinyl)pyrimidine (142 mg, 56%). LCMS: (M+H)+: 277.0.

Provenance & Evidence